A multi-kinase inhibitor; inhibits B-RAF

CCT241161 – 5 mg

Brand:
Cayman
CAS:
1163719-91-2
Storage:
-20
UN-No:
Non-Hazardous - /

CCT241161 is a multi-kinase inhibitor that inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 252, 15, 6, 15, and 3 nM, respectively).{41909} It is selective for RAFs, Src, LCK, and MAPKs in a panel of 63 kinases when used at a concentration of 1 µM. CCT241161 inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells, but not B-RAF wild-type D35 cells, and inhibits growth of B-RAF mutant melanoma cells in a concentration-dependent manner. In vivo, CCT241161 (20 mg/kg per day) induces tumor regression in a B-RAF mutant A375 mouse xenograft model. CCT241161 also inhibits ERK and Src signaling and induces tumor regression in B-RAF inhibitor-resistant patient-derived xenograft (PDX) mouse models including those resistant to both dabrafenib (Item No. 16989) and trametinib (Item No. 16292).  

 

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Description

A multi-kinase inhibitor; inhibits B-RAF, B-RAFV600E, C-RAF, Src, and LCK (IC50s = 252, 15, 6, 15, and 3 nM, respectively); only inhibits RAFs, Src, LCK, and MAPKs in a panel of 63 kinases at 1 µM; inhibits MEK and ERK signaling in B-RAF mutant WM266.4 cells; inhibits growth of B-RAF mutant melanoma cells; induces tumor regression in a B-RAF mutant A375 mouse xenograft model at 20 mg/kg per day; inhibits ERK and Src signaling and induces tumor regression in B-RAF inhibitor-resistant PDX mouse models

Formal name: N-[4-[(3,4-dihydro-3-oxopyrido[2,3-b]pyrazin-8-yl)oxy]-2-(methylthio)phenyl]-N’-[3-(1,1-dimethylethyl)-1-phenyl-1H-pyrazol-5-yl]-urea

Synonyms: 

Molecular weight: 541.6

CAS: 1163719-91-2

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Cancer|Cell Signaling|SRC Family Signaling

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